Abstract
Background: Cancer is a serious health concern worldwide making the continuous discovery of new cytotoxic agents a challenging issue. In this study, the cytotoxicity of a naturally occurring alkenylmethylresorcinol, ardisinol III was evaluated in a panel of six human carcinoma cell lines and the normal fibroblasts.
Methods: The cytotoxicity of samples was evaluated by the neutral red uptake (NR) assay; the activity of caspases in breast adenocarcinoma MCF7 cells was detected by caspase-Glo assay; flow cytometry was used to analyze the cell cycle and mitochondrial membrane potential (MMP), and spectrophotometry was used to measure levels of reactive oxygen species (ROS).
Results: Ardisinol III had IC50 values below 10 µM in all the six tested carcinoma cell lines. The obtained IC50 values ranged from 0.88 µM (against SPC212 mesothelioma cells) to 8.36 µM (against hepatocarcinoma HepG2 cells). Ardisinol III was less toxic in normal CRL2120 fibroblasts and the selectivity indexes in all cell lines were above 6. This alkenylmethylresorcinol induced apoptosis in MCF7 breast adenocarcinoma cells, through activation of caspases 3/7 and 9, loss of MMP and increase ROS production.
Conclusions: Ardisinol III is a cytotoxic molecule that deserves to be further explored as a potential anticancer agent to combat human carcinoma.
Keywords: alkenylmethylresorcinol; ardisinol III; carcinoma; cytotoxicity; mode of action.
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